Kapetanovic I M, Crowell J A, Krishnaraj R, Zakharov A, Lindeblad M, Lyubimov A
Chemopreventive Agent Development Research Group, Division of Cancer Prevention, National Cancer Institute, Bethesda, MD 20892, USA.
Toxicology. 2009 Jun 16;260(1-3):28-36. doi: 10.1016/j.tox.2009.03.007. Epub 2009 Mar 24.
Standardized green tea extract was evaluated for exposure and toxicity in Beagle dogs following oral dosing by capsules. The main component (-)-epigallocatechin gallate (EGCG) accounted for 56-72% of the material. A 9-month chronic study (0, 200, 500, and 1000 mg/kg/day) was done in fasted dogs to take advantage of the reported improved catechin bioavailability with fasting. Extensive morbidity, mortality, and pathology of many major organs led to its early termination at 6.5 months and prevented identification of the toxicity mechanisms. A follow-up 13-week study examined the exposure to and toxicity of the extract. In general, toxicities were less severe than in the chronic study during the same interval. Dosing in a fed state resulted in considerably lower and less variable exposure than found under fasted conditions. Toxicity was less frequent and of lesser severity with lower exposure but limited sample size and large variability prevented reaching that definitive conclusion. Differences in mortality and morbidity between the preliminary terminated chronic and follow-up subchronic studies with the same dose of the same drug lot and similar exposure were not fully resolved as there may be other as yet unclear confounding factors.
通过胶囊口服给药后,对标准绿茶提取物在比格犬中的暴露情况和毒性进行了评估。主要成分(-)-表没食子儿茶素没食子酸酯(EGCG)占该物质的56 - 72%。在禁食的犬中进行了一项为期9个月的慢性研究(剂量为0、200、500和1000 mg/kg/天),以利用所报道的禁食可提高儿茶素生物利用度这一情况。许多主要器官出现广泛的发病、死亡和病理变化,导致该研究在6.5个月时提前终止,且无法确定毒性机制。一项为期13周的后续研究考察了该提取物的暴露情况和毒性。总体而言,在相同时间段内,毒性不如慢性研究中严重。与禁食条件下相比,在进食状态下给药导致的暴露量显著更低且变异性更小。暴露量较低时,毒性发生频率较低且严重程度较轻,但样本量有限和变异性较大阻碍了得出明确结论。由于可能存在其他尚不清楚的混杂因素,同一药物批次相同剂量且暴露情况相似的初步终止的慢性研究与后续亚慢性研究之间的死亡率和发病率差异尚未完全解决。